rat microsomal

CVT-12012 is an orally bioavailable inhibitor of stearoyl-CoA desaturase (SCD; IC50 = 6.1 nM in HepG2 cells).

RPR107393 free base is a selective and potent inhibitor of squalene synthase (SQS) for the study of neurological disorders and endocrine and metabolic disorders.

SC-26196 is an orally active inhibitor of Delta6 desaturase (D6D) with IC50 of 0.2 µM in a rat liver microsomal assay, with antiinflammatory properties.

Beauvericin, a Fusarium mycotoxin, inhibits acyl-CoA:cholesterol acyltransferase (ACAT) in rat liver microsomal enzyme assays with an IC50 value of 3 μM.

G256 (Compound 1) is a guanidinyl hydrazone and can also be considered a Schiff base of aminoguanidine. It exhibits antiarrhythmic activity. G256 is the reduced form of NOH-G256, prepared from rabbit and rat liver homogenates using microsomal enzymes in the presence of NADPH and NADH.

Quindoxin is a potent antibacterial agent that has been rigorously evaluated for genetic toxicity using the Salmonella microsomal assay system, where experimental testing demonstrated that this compound induces both base pair substitution mutations and frameshift mutations in Salmonella strains independently of the presence of a rat liver microsomal fraction, with mutagenic activity shown to be mechanistically dependent on the presence of its N-oxide functional group, as fully reduced quinoxaline lacked mutagenicity while partially reduced quinoxaline-N-oxide displayed diminished activity, and recA- and uvrB-deficient Salmonella strains exhibited increased susceptibility compared with wild-type strains.

Dehydro warfarin, a metabolite of (±)-warfarin, is formed by rat liver microsomes from (±)-warfarin.

9(E)-Octadecenamide (Elaidamide) is a fatty acid amide and endogenous metabolite that inhibits rat microsomal epoxide hydrolase (mEH) with a Ki of 70 nM.

UDP-glucosamine disodium is a sugar nucleotide analogue. UDP-glucosamine disodium acts as a sugar donor in microsomal preparations of both chick-embryo cells and rat liver, yielding dolichyl monophosphate glucosamine (Dol-P-GlcN).

Gypsetin inhibits the activity of acyl-CoA:cholesterol acyltransferase (ACAT), showing inhibitory effects on rat liver microsomal ACAT with an IC50 of 18 μM, and competes with oleoyl-CoA substrate, possessing a Ki value of 5.5 μM. Additionally, Gypsetin prevents the formation of cholesterol esters from oleic acid with an IC50 of 0.65 μM.

Epicochlioquinone A inhibits rat liver microsomal ACAT with an IC50 of 1.7 μM and inhibits plasma lecithin-cholesterol acyltransferase (LCAT) with an IC50 of 15.8 μM. At a dosage of 75 mg/kg, it can reduce cholesterol absorption in rats by 50%.